Abstract：
BACKGROUND: Fullerenes C60 shows great potential for drug transport. C60 generates large amounts of singlet oxygen upon photoexcitation, which has a significant inhibitory effect on tumor cells, so the photosensitive properties of C60 were exploited for photodynamic therapy of tumors by laser irradiation.
METHODS: In this study, C60-NH2 was functionalized by introducing amino acids on the surface of C60, coupled with 5-FU to obtain C60 amino acid-derived drugs (C60AF, C60GF, C60LF), and activated photosensitive drugs (C60AFL, C60GFL, C60LFL) were obtained by laser irradiation. The C60 nano-photosensitive drugs were characterized in various ways, and the efficacy and safety of C60 nano-photosensitive drugs were verified by cellular experiments and animal experiments. Bioinformatics methods and cellular experiments were used to confirm the photosensitive drug targets and verify the therapeutic targets with C60AF.
RESULTS: Photosensitised tumor-targeted drug delivery effectively crosses cell membranes, leads to more apoptotic cell death, and provides higher anti-tumor efficacy and safety in vitro and in vivo colorectal cancer pharmacodynamic assays compared to free 5-FU.C60 photosensitized drug promotes tumor killing by inhibiting the colorectal cancer FLOR1 tumor protein target, with no significant toxic effects on normal organs.
CONCLUSIONS: C60 photosensitized drug delivery systems are expected to improve efficacy and reduce side effects in the future treatment of colorectal cancer. Further and better development and design of drugs and vectors for colorectal cancer therapy.
METHODS: In this study, C60-NH2 was functionalized by introducing amino acids on the surface of C60, coupled with 5-FU to obtain C60 amino acid-derived drugs (C60AF, C60GF, C60LF), and activated photosensitive drugs (C60AFL, C60GFL, C60LFL) were obtained by laser irradiation. The C60 nano-photosensitive drugs were characterized in various ways, and the efficacy and safety of C60 nano-photosensitive drugs were verified by cellular experiments and animal experiments. Bioinformatics methods and cellular experiments were used to confirm the photosensitive drug targets and verify the therapeutic targets with C60AF.
RESULTS: Photosensitised tumor-targeted drug delivery effectively crosses cell membranes, leads to more apoptotic cell death, and provides higher anti-tumor efficacy and safety in vitro and in vivo colorectal cancer pharmacodynamic assays compared to free 5-FU.C60 photosensitized drug promotes tumor killing by inhibiting the colorectal cancer FLOR1 tumor protein target, with no significant toxic effects on normal organs.
CONCLUSIONS: C60 photosensitized drug delivery systems are expected to improve efficacy and reduce side effects in the future treatment of colorectal cancer. Further and better development and design of drugs and vectors for colorectal cancer therapy.
摘要：
背景：富勒烯C60显示出巨大的药物转运潜力。C60在光激发时产生大量的单线态氧，对肿瘤细胞有显著的抑制作用，因此，C60的光敏特性被用于激光照射肿瘤的光动力治疗。
方法：在本研究中，通过在C60表面引入氨基酸使C60-NH2功能化，与5-FU偶联，获得C60氨基酸衍生药物(C60AF，C60GF,C60LF),和活化的光敏药物(C60AFL，C60GFL,C60LFL)通过激光辐照获得。对C60纳米光敏药物进行了多种表征,细胞实验和动物实验验证了C60纳米光敏药物的有效性和安全性。生物信息学方法和细胞实验用于确认光敏药物靶标并验证C60AF的治疗靶标。
结果：光敏化的肿瘤靶向药物递送有效地穿过细胞膜，导致更多的凋亡性细胞死亡，并且与游离5-FU相比,在体外和体内结肠直肠癌药效学测定中提供更高的抗肿瘤功效和安全性。C60光敏化药物通过抑制大肠癌FLOR1肿瘤蛋白靶点促进肿瘤杀伤,对正常器官无明显毒性作用。
结论：C60光敏化给药系统有望在未来结直肠癌的治疗中提高疗效并减少副作用。进一步更好地开发和设计用于结直肠癌治疗的药物和载体。
方法：在本研究中，通过在C60表面引入氨基酸使C60-NH2功能化，与5-FU偶联，获得C60氨基酸衍生药物(C60AF，C60GF,C60LF),和活化的光敏药物(C60AFL，C60GFL,C60LFL)通过激光辐照获得。对C60纳米光敏药物进行了多种表征,细胞实验和动物实验验证了C60纳米光敏药物的有效性和安全性。生物信息学方法和细胞实验用于确认光敏药物靶标并验证C60AF的治疗靶标。
结果：光敏化的肿瘤靶向药物递送有效地穿过细胞膜，导致更多的凋亡性细胞死亡，并且与游离5-FU相比,在体外和体内结肠直肠癌药效学测定中提供更高的抗肿瘤功效和安全性。C60光敏化药物通过抑制大肠癌FLOR1肿瘤蛋白靶点促进肿瘤杀伤,对正常器官无明显毒性作用。
结论：C60光敏化给药系统有望在未来结直肠癌的治疗中提高疗效并减少副作用。进一步更好地开发和设计用于结直肠癌治疗的药物和载体。
